Niclosamide

Pricing Availability   Qty
Description: STAT3 inhibitor; also inhibits mTORC1 signaling
Chemical Name: 5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews
Pathways (1)

Biological Activity for Niclosamide

Niclosamide is an inhibitor of the STAT3 signaling pathway; inhibits the activation, nuclear translocation and transactivation of STAT3. Niclosamide displays selectivity for STAT3 over STAT1, STAT5, JAK1, JAK2 and Src kinases. It inhibits the transcription of STAT3 target genes and induces cell growth inhibition, apoptosis and cell cycle arrest of cancer cells with constitutively active STAT3. It also reversibly inhibits mTORC1 signaling and stimulates autophagy in vitro; displays antineoplastic effects in acute myelogenous leukemia (AML) stem cells. In addition, niclosamide inhibits SARS-CoV-2 replication in vitro (IC50 = 0.34 μM in Vero E6 plaque assay) through suppression of TMEM16F activity.

Technical Data for Niclosamide

M. Wt 325.99
Formula C13H8Cl2N2O4
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 50-65-7
PubChem ID 4477
InChI Key RJMUSRYZPJIFPJ-UHFFFAOYSA-N
Smiles O=C(NC2=C(Cl)C=C([N+]([O-])=O)C=C2)C1=C(O)C=CC(Cl)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Niclosamide

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 8.15 25
DMSO 3.26 10

Preparing Stock Solutions for Niclosamide

The following data is based on the product molecular weight 325.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 12.27 mL 61.35 mL 122.7 mL
1.25 mM 2.45 mL 12.27 mL 24.54 mL
2.5 mM 1.23 mL 6.14 mL 12.27 mL
12.5 mM 0.25 mL 1.23 mL 2.45 mL

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References for Niclosamide

References are publications that support the biological activity of the product.

Balgi et al (2009) Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4 e7124 PMID: 19771169

Jin et al (2010) Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-κB pathway and generation of reactive oxygen species. Cancer Res. 70 2516 PMID: 20215516

Ren et al (2010) Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway. ACS Med.Chem.Lett. 1 454 PMID: 24900231

Braga et al (2021) Drugs that inhibit TMEM16 proteins block SARS-CoV-2 spike-induced syncytia. Nature 594 88 PMID: 33827113


If you know of a relevant reference for Niclosamide, please let us know.

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Keywords: Niclosamide, Niclosamide supplier, STAT3, mTORC1, signaling, signalling, pathway, inhibitors, inhibits, anthelmintic, SARS-CoV-2, spike, TMEM16F, STAT, mTOR, Stem, Cell, Signaling, Autophagy, Cancer, Cells, Coronavirus, Ca2+-Activated, Chloride, Channels, 4079, Tocris Bioscience

4 Citations for Niclosamide

Citations are publications that use Tocris products. Selected citations for Niclosamide include:

Natarajan et al (2014) STAT3 modulation to enhance motor neuron differentiation in human neural stem cells. PLoS One 9 e100405 PMID: 24945434

Ru-Rong et al (2020) Periostin Activation of Integrin Receptors on Sensory Neurons Induces Allergic Itch. Cell Rep 31 107472 PMID: 32268102

Yan et al (2021) A Novel Biological Activity of the STAT3 Inhibitor Stattic in Inhibiting Glutathione Reductase and Suppressing the Tumorigenicity of Human Cervical Cancer Cells via a ROS-Dependent Pathway. Onco Targets Ther 14 4047-4060 PMID: 34262291

Eun-Kyoung et al (2017) The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells. Int J Mol Sci 18 PMID: 29077055


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Pathways for Niclosamide

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.